Assay Detail
Binding
CHEMBL770981
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory effect against recombinant human protein-tyrosine phosphatase 1B (PTP1B), using p-nitrophenyl phosphate substrate at pH 5.5.
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Tyrosine-protein phosphatase non-receptor type 1 (CHEMBL335) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and SAR of a novel selective and orally bioavailable nonpeptide classical competitive inhibitor class of protein-tyrosine phosphatase 1B.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 44 | 5.30 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL140120 | — | — | 1 | 6.57 |
| CHEMBL139393 | — | — | 1 | 6.54 |
| CHEMBL137989 | — | — | 1 | 6.16 |
| CHEMBL140757 | — | — | 1 | 6.05 |
| CHEMBL136044 | — | — | 1 | 6.00 |
| CHEMBL138277 | — | — | 1 | 6.00 |
| CHEMBL138951 | — | — | 1 | 6.00 |
| CHEMBL138240 | — | — | 1 | 5.96 |
| CHEMBL138025 | — | — | 1 | 5.89 |
| CHEMBL136316 | — | — | 1 | 5.75 |
| CHEMBL139356 | — | — | 1 | 5.70 |
| CHEMBL341558 | — | — | 1 | 5.66 |
| CHEMBL138257 | — | — | 1 | 5.60 |
| CHEMBL337759 | — | — | 1 | 5.35 |
| CHEMBL141481 | — | — | 1 | 5.33 |
| CHEMBL139422 | — | — | 1 | 5.29 |
| CHEMBL139590 | — | — | 1 | 5.21 |
| CHEMBL343587 | — | — | 1 | 5.21 |
| CHEMBL423546 | — | — | 1 | 5.10 |
| CHEMBL139491 | — | — | 1 | 5.10 |
| CHEMBL342478 | — | — | 1 | 5.10 |
| CHEMBL138152 | — | — | 1 | 5.09 |
| CHEMBL139423 | — | — | 1 | 5.08 |
| CHEMBL336894 | — | — | 1 | 5.05 |
| CHEMBL139923 | — | — | 1 | 5.00 |
| CHEMBL138575 | — | — | 1 | 4.96 |
| CHEMBL138151 | — | — | 1 | 4.92 |
| CHEMBL139024 | — | — | 1 | 4.92 |
| CHEMBL139489 | — | — | 1 | 4.92 |
| CHEMBL137867 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL140120 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL139393 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL137989 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL140757 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL136044 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL138277 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL138951 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL138240 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL138025 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL136316 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL139356 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL341558 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL138257 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL337759 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL141481 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL139422 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL139590 | — | Ki | = | 6100.0 | nM | 5.21 |
| CHEMBL343587 | — | Ki | = | 6100.0 | nM | 5.21 |
| CHEMBL423546 | — | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL139491 | — | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL342478 | — | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL138152 | — | Ki | = | 8100.0 | nM | 5.09 |
| CHEMBL139423 | — | Ki | = | 8300.0 | nM | 5.08 |
| CHEMBL336894 | — | Ki | = | 9000.0 | nM | 5.05 |
| CHEMBL139923 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL138575 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL138151 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL139024 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL139489 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL137867 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL336435 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL344412 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL138806 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL343979 | — | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL341806 | — | Ki | = | 18000.0 | nM | 4.75 |
| CHEMBL139050 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL344585 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL138659 | — | Ki | = | 26000.0 | nM | 4.58 |
| CHEMBL336879 | — | Ki | = | 37000.0 | nM | 4.43 |
| CHEMBL138406 | — | Ki | = | 160000.0 | nM | - |
| CHEMBL342612 | — | Ki | = | 108000.0 | nM | - |
| CHEMBL337326 | — | Ki | = | 1700000.0 | nM | - |
| CHEMBL140929 | — | Ki | = | 2000000.0 | nM | - |
| CHEMBL337132 | — | Ki | = | 1100000.0 | nM | - |